Betaxolol
Generic Name: betaxolol hydrochloride
Brand Name: Kerlone
Indications
Betaxolol is indicated in the treatment of hypertension.
Dosage and Administration
Betaxolol is a b1-selective (cardioselective) adrenergic receptor blocking agent available as 10-mg and 20-mg tablets for oral administration.
Normal Dosage: recommended initial dose of Betaxolol is normally 10 mg once daily. The full antihypertensive effect is usually seen within 7 to 14 days.
Overdose?
The most common effects seen are congestive heart failure, hypotension, bronchospasm, hypoglycemia. In such cases, treatment with Betaxolol should be stopped and the patient carefully observed.
Drug Description
Kerlone is chemically described as 2-propanol, 1-[4-[2-(cyclopropylmethoxy) ethyl] phenoxy]-3-[(1-methylethyl) amino]-, hydrochloride, (±). Betaxolol hydrochloride is a water-soluble white crystalline powder with a molecular formula of C18H29NO3-HCl and a molecular weight of 343.9. It is freely soluble in water, ethanol, chloroform, and methanol, and has a pKa of 9.4.
Side Effects
Some of the noted side effects are headache, dizziness, fatigue, lethargy, nervousness, nausea, diarrhea, chest pain, and rash.
Precautions
- Bronchospastic and diabetic patients need to use Betaxolol with utmost caution.
- Caution should be exercised when Kerlone is administered to a nursing mother.
- Safety and effectiveness in pediatric patients have not been established.
Drug Interactions
- Alpha-blockers (prazosin, terazosin): Concurrent use of beta-blockers may increase risk of orthostasis.
- CYP1A2 inducers: May decrease the levels/effects of betaxolol. Example inducers include aminoglutethimide, carbamazepine, phenobarbital, and rifampin.
- CYP1A2 inhibitors: May increase the levels/effects of betaxolol. Example inhibitors include amiodarone, ciprofloxacin, fluvoxamine, ketoconazole, norfloxacin, ofloxacin, and rofecoxib.
- CYP2D6 inhibitors: May increase the levels/effects of betaxolol. Example inhibitors include chlorpromazine, delavirdine, fluoxetine, miconazole, paroxetine, pergolide, quinidine, quinine, ritonavir, and ropinirole.
- Clonidine; Hypertensive crisis after or during withdrawal of either agent.
- Drugs which slow AV conduction (digoxin): Effects may be additive with beta-blockers.
- Glucagon: Betaxolol may blunt the hyperglycemic action of glucagon.
- Insulin and oral hypoglycemics: May mask tachycardia from hypoglycemia.
- NSAIDs (ibuprofen, indomethacin, naproxen, piroxicam) may reduce the antihypertensive effects of beta-blockers.
- Salicylates may reduce the antihypertensive effects of beta-blockers.
- Sulfonylureas: Beta-blockers may alter response to hypoglycemic agents.
- Verapamil or diltiazem may have synergistic or additive pharmacological effects when taken concurrently with beta-blockers.
